Anxiolytic psychotropic drugs: their characteristics and effects.

A summary of the characteristics of anxiolytics: the effects and uses of these drugs.

Anxiolytic psychotropic drugs are medications that have contributed greatly to the treatment of anxiety and sleep problems, as well as pain associated with chronic diseases such as fibromyalgia or fibromyalgia.They are also used to treat pain associated with chronic illnesses such as fibromyalgia or accidents.

These drugs, as with all other drugs, have their advantages and risks, working very well if taken as prescribed by a psychiatrist and being genuinely dangerous if abused.

Next we will see this extensive family of drugs, some examples of them, their main mechanisms of action and what happens when they are abused.

What are anxiolytics?

Throughout history, all kinds of natural substances have been used to try to calm and soothe, especially in the form of infusions such as chamomile, valerian, lime blossom or lemon verbena. However, thanks to chemical and pharmacological advances since the mid-nineteenth century, all kinds of psychotropic drugs have been introduced as treatments for anxiety and sleep disorders, replacing both infusions and other treatments such as alcohol and opium derivatives.

As is the case with all other psychotropic drugs, anxiolytics are medications whose main function is to affect certain neurons in the central nervous systemin this case those that induce anxiety and insomnia. Anxiolytics calm nervousness by influencing, directly or indirectly, the way in which these nerve cells release and reuptake certain neurotransmitters.

The main effect of anxiolytics, together with sedatives, is to act on the central nervous system by depressing it, i.e. they reduce brain activity associated with the origin of the symptoms. act on the central nervous system by depressing it, i.e. they reduce the brain activity associated with the origin of the symptoms of anxiety. symptoms of anxiety. In the case of anxiolytics, they reduce the signs of anxiety and agitation without producing numbness, while sedatives do have a clear hypnotic effect, reducing the level of consciousness. Similarly, both types of drugs can be used as tranquilizers.

Because anxiolytics are relatively easy to obtain, their consumption has been increasing in recent decades, making them one of the most widely prescribed drugs in psychiatric practice. Nowadays its consumption is present in all social sectors, often seen as a cheaper, faster and easier option to solve anxiety problems than psychological therapy, although they do not really eliminate the cause, but the symptom.

Classification

The family of anxiolytics does not correspond to a group of drugs that share chemical characteristics, but rather their effects.. Among the anxiolytics we can find drugs as diverse as benzodiazepines, barbiturates and barbiturate analogues.

Benzodiazepines

Benzodiazepines are prescribed for short-term relief of highly disabling anxiety at pathological levels. These drugs produce a sedative-hypnotic effect..

Benzodiazepines are usually prescribed for short-term relief of highly disabling anxiety. These are drugs that, despite being quite safe, have the capacity to generate very high tolerance and dependence, which translates into a greater likelihood of addiction.

All benzodiazepines act by increasing the action of the neurotransmitter GABA (gamma-aminobutyric acid).. This neurotransmitter is responsible for transmitting inhibitory messages from one neuron to another, i.e. causing nerve cells to slow down or stop transmitting.

Depending on the duration of their half-life we can speak of up to four types of benzodiazepines:

1. ultra-short duration benzodiazepines.

Their half-life is less than 6 hours. Among them we can find Brotizolam. N-fidazolain.

2. Benzodiazepines of short duration

Their half-life is between 6 and 12 hours.. They have few residual effects if taken before going to bed at night, although their too frequent use can cause rebound insomnia and anxiety upon awakening. Among them we can find: Loprazolam, Oxazepam and Temazepam.

3. Benzodiazepines of intermediate duration

Their half-life ranges from 12 to 24 hours.. Some residual effects may occur during the first half of the day. Rebound insomnia tends to be more frequent when use is stopped abruptly and without adequate medical supervision. As a result, some withdrawal symptoms may occur during the day, especially if they have been taken for a long period of time.

Among the intermediate-acting benzodiazepines we find: Alprazolam and Bromazepam, Lorazepam.

4. Long-acting benzodiazepines

Their half-life is longer than 24 hours. They have very potent sedative effects, which tend to last during the following day if they are used to treat insomnia.

Their half-life is greater than 24 hours. Their sedative effects are very potent, so they tend to last during the day after they are used to treat insomnia.

Among these benzodiazepines we find: Clonazepam, Clobazepam, Chlorazepate, Diazepam and Ketazolam.

Z-drugs

Z-drugs, also called benzodiazepine analogs, are drugs whose chemical structure is different from that of benzodiazepines but have a similar pharmacological action.. For this reason, they usually have the same therapeutic indications as their analogues, and curiously, they have the same side effects and involve the same risks. These peculiar drugs are three: Zolpidem, Zopiclone and Zaleplon.

Barbiturates

Barbiturates are drugs that reduce anxiety due to their potent sedative effect..

They have a rather bad reputation since they are known for their high risk of abuse and addiction, so that their use is currently discouraged to treat anxiety. Among them we find Amobarbital, Butalbital, Phenobarbital, Secobarbital and Pentobarbital.

Pharmacologically speaking, they behave as agonists of GABA-A receptors.receptors, although they also act at other levels, such as antagonizing the excitatory effect of glutamic acid and in high doses interfering with the transport of calcium, sodium and potassium ions across the neuronal membrane, which has been related to their greater intensity compared to benzodiazepines.

Azapirones

Azapirones include buspirone, gepirone, ipsapirone and tandospirone, drugs with moderate anxiolytic capacity that only manifests itself when administered chronically.. They have also been used as antidepressants.

They are partial agonists of the 5-HT receptors so their action is focused on the their action is focused on the regulation of serotonergic neurotransmission, without affecting serotonergic neurotransmissionwithout affecting GABAergic neurotransmission. They cannot be used as hypnotics since they lack direct sedative effect.

Effects of anxiolytics

As their name suggests, anxiolytics are prescribed to treat anxiety. The effects and intensity depend on the type of drug taken, the dose and the characteristics of the drug itself.The effects and intensity depend on the type of drug taken, the dosage and the person's own characteristics, especially his or her ability to eliminate the drug.

In the case of benzodiazepines, at low doses they reduce restlessness, emotional tension and anxiety, without altering sensory perception or alertness too much. At medium doses they produce calmness and drowsiness and may even cause some momentary speech difficulties. At high doses, benzodiazepines produce unconsciousness, which is why they are used as surgical anesthesia.which is why they are used as surgical anesthesia.

Side effects

Each anxiolytic drug has its own side effects, directly linked to the dose, mechanism of action and the time it takes for them to be eliminated from the body. However, we can find that many of the adverse effects of these drugs coincide, especially those effects that areThe most common side effects of these drugs coincide, especially those effects that are related to anxiety and state of consciousness, either increasing or reducing them to problematic levels. The most common side effects of these drugs are.

• Dry mouth and nose
• Dysgeusia: metallic taste sensation.
• Mydriasis: pupil dilation
• Constipation
• Blurred vision
• Dizziness
• Nausea
• Restlessness
• Tremors
• Loss of sexual desire
• Erection problems in men

In the specific case of benzodiazepines, their long-term side effects are of great concern, as they can cause permanent physical and psychological as they can cause permanent physical and psychological alterations. Long-term use causes sexual dysfunction, damage to the cerebellum, skin rashes, joint pain, headaches, low Blood pressure, heart attacks, liver and kidney poisoning, tremors, vertigo and severe psychological deterioration.

The mixture of anxiolytic psychotropic drugs with other drugs, both anxiolytic and non-anxiolytic, and drugs can be very dangerous. It is true that in clinical practice all kinds of drugs are combined, but these combinations are controlled and studied by psychiatrists, who know how these drugs interact and what benefits they will bring to the patient.

It is especially inadvisable to mix benzodiazepines with alcohol. since their effects do not add up, but multiply in such an uncontrolled and life-threatening way. Among the symptoms that may appear from this explosive combination are cardiorespiratory arrest and loss of consciousness, although, ironically, anxious symptoms such as high excitability, hostile reactions and aggressiveness may also occur.

Anxiolytic Withdrawal Syndrome

A little known effect of anxiolytic psychotropic drugs is a picture that resembles that of an alcohol hangover. This appears especially if the medication has been abused, consuming it in large doses..

Benzodiazepines usually cause high tolerance and dependence, causing the person to consume larger and larger doses, since the therapeutic effects are reduced over time. When treatment is stopped abruptly, anxious symptoms and excitement appear even more intense than when the treatment started, which makes the person, in case he/she gets new drugs, use them again and fall into an addiction.

The degree of dependence on anxiolytics will depend on the type of drug taken, the dose consumed and the length of time it has been used. The withdrawal syndrome manifests itself with the following symptoms.

• Perceptual disturbances
• Fainting
• Restlessness
• Constant nervousness
• Tremors
• Weakness
• Nausea
• Vomiting
• Headache
• Hyperactivity to external stimuli
• Nystagmus: rapid eye movements without being able to control them.

In most cases, people who develop addiction to anxiolytics and sedatives started taking them for medical reasons.The dependence can develop in a very short period of time, in as little as two weeks of constant use, such as having anxious symptoms, insomnia or pain associated with an accident or chronic illness such as fibromyalgia. Dependence can develop in a very short time, in as little as two weeks of constant use.

Considering the seriousness of the withdrawal syndrome associated with anxiolytic psychotropic drugs it is very important to be under the supervision of a physician when starting treatment with these drugs.. He/she will dose the drug, will prescribe how to take it and, if the two weeks are exceeded, will initiate the withdrawal by means of a progressive reduction of the dose, never all at once.

Overdose and treatment

Overdose by anxiolytic psychopharmaceuticals gives rise to a picture with the following symptoms, in addition to being life-threatening.

• Drowsiness
• Confusion
• Respiratory depression
• Slurred speech
• Stupor: difficulty to be awakened.
• Poor coordination
• Confusion

In the elderly, symptoms can be more severe and may include:

• Dizziness
• Disorientation,
• Delirium
• Loss of balance: causes bone breakage, especially of the hip.

If benzodiazepines have been overdosed, this is a truly dangerous condition.. The person may go into a coma, have a serious alteration of the respiratory and cardiac function and, in addition, may end up dying. It should be noted that although this is relatively difficult to happen, since the therapeutic dose is usually much lower than the potentially fatal dose in the case of benzodiazepines, this must be taken into account, especially in surgical practice.

Serious or life-threatening symptoms from benzodiazepines are unlikely compared to barbiturates, because benzodiazepines are usually prescribed at doses farther away from dangerous doses, with a significant margin of safety. People can take relatively large amounts of benzodiazepines on their own and not die.

It is a different matter in surgical practiceThe amounts of benzodiazepines are much higher than those prescribed in psychiatry.

In case the overdose was caused by the benzodiazepine, the antidote drug used is flumazenil, which can reverse a severe overdose. However, this drug can trigger benzodiazepine withdrawal and cause seizures in people who have taken benzodiazepines for a long time. Therefore, flumazenil is not usually administered routinely for overdose. In barbiturate overdoses, physicians may administer sodium bicarbonate intravenously to help the person excrete the barbiturate in the urine.

Bibliographic references:

• Adán, A. and Prat, G. (2016). Psychopharmacology: mechanism of action, effect and therapeutic management. Barcelona, Spain. Marge Medica Books.
• Gómez-Jarabo, G. (1999). Pharmacology of behavior. Basic manual for psychotherapists and clinicians. Madrid: Síntesis psicología.
• Morón, F.G.; Borroto,R.; Calvo, D.M.; Cires, M.; Cruz, M.A. and Fernández, A. (2009). Clinical pharmacology. Havana: Editorial Ciencias Médicas; 1-30.
• Stevens, J.C. & Pollack, M.H. (2005). Benzodiazepines in clinical practice: consideration of their long-term use and alternative agents. J Clin Psychiatry; 66 (Suppl 2):21-7.